DPM2 Inhibitors
Chemical inhibitors of dolichol-phosphate mannose synthase subunit 2 (DPM2) disrupt its role in the N-linked glycosylation pathway through various mechanisms. Tunicamycin is one such inhibitor, which directly hampers the formation of dolichol-linked oligosaccharides by inhibiting the transfer of N-acetylglucosamine to dolichol phosphate, a crucial step in the synthesis of the glycan precursor. This action results in a blockade of the glycosylation pathway at an early stage, indirectly inhibiting the function of DPM2. Swainsonine and kifunensine target mannosidase II and mannosidase I, respectively. By inhibiting these glycosylation-processing enzymes, these compounds prevent the proper formation and trimming of oligosaccharides, processes in which DPM2 is indirectly involved. This results in an accumulation of misprocessed glycans, which can interfere with the functions of DPM2.
Moreover, other inhibitors like castanospermine, deoxynojirimycin, and N-butyldeoxynojirimycin interfere with glucosidases I and II. These enzymes are responsible for cleaving glucose residues from the N-linked glycosylation precursor, and their inhibition leads to improper glycan assembly. This, in turn, can inhibit the functional activity of DPM2. Brefeldin A disrupts the structure and function of the Golgi apparatus, essential for the later stages of glycoprotein processing and transport. As DPM2 is integral in the synthesis of glycan structures within the ER-Golgi network, the disruption caused by Brefeldin A impairs the environment necessary for DPM2 activity. AMP-DNM and celgosivir further expand the list of chemical inhibitors by targeting the synthesis of GDP-mannose and alpha-glucosidases, respectively. AMP-DNM's competitive inhibition of GDP-mannose synthesis limits the availability of substrates crucial for DPM2 function, while celgosivir, a prodrug of castanospermine, inhibits the enzymes essential for the initial glycosylation steps. All these inhibitors collectively contribute to the functional suppression of DPM2 by targeting different enzymes and steps within the glycosylation pathway.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Tunicamycin | 11089-65-9 | sc-3506A sc-3506 | 5 mg 10 mg | $169.00 $299.00 | 66 | |
Tunicamycin inhibits N-linked glycosylation by blocking the transfer of N-acetylglucosamine to dolichol phosphate, which is a precursor required for the synthesis of the glycan precursor. DPM2, being a subunit of dolichol-phosphate mannose synthase complex, is implicated in glycosylation; inhibition of this precursor synthesis can lead to functional inhibition of DPM2. | ||||||
Swainsonine | 72741-87-8 | sc-201362 sc-201362C sc-201362A sc-201362D sc-201362B | 1 mg 2 mg 5 mg 10 mg 25 mg | $135.00 $246.00 $619.00 $799.00 $1796.00 | 6 | |
Swainsonine inhibits mannosidase II, an enzyme involved in the trimming of the oligosaccharide precursor. This disruption in the processing of N-glycans can indirectly inhibit the functional activity of DPM2 by preventing the proper formation of the glycosyl structures that DPM2 is involved in assembling. | ||||||
Castanospermine | 79831-76-8 | sc-201358 sc-201358A | 100 mg 500 mg | $180.00 $620.00 | 10 | |
Castanospermine inhibits glucosidase I and II, enzymes responsible for the cleaving of glucose residues from the N-linked glycosylation precursor. By inhibiting these enzymes, castanospermine can indirectly inhibit DPM2 by impairing the initial steps of glycan assembly, which DPM2 is crucial for. | ||||||
Deoxynojirimycin | 19130-96-2 | sc-201369 sc-201369A | 1 mg 5 mg | $72.00 $142.00 | ||
Deoxynojirimycin inhibits glucosidase I, which is essential for the proper folding of glycoproteins. This inhibition can lead to the accumulation of misfolded glycoproteins, which indirectly can inhibit DPM2 by disrupting the glycosylation process in which DPM2 is involved. | ||||||
Deoxymannojirimycin hydrochloride | 84444-90-6 | sc-201360 sc-201360A | 1 mg 5 mg | $93.00 $239.00 | 2 | |
Deoxymannojirimycin inhibits mannosidase I, an enzyme involved in the processing of N-linked glycans. By inhibiting this enzyme, the maturation of glycosylation intermediates is disrupted, which can functionally inhibit DPM2 due to its role in the synthesis of the glycan structures. | ||||||
Kifunensine | 109944-15-2 | sc-201364 sc-201364A sc-201364B sc-201364C | 1 mg 5 mg 10 mg 100 mg | $132.00 $529.00 $1005.00 $6125.00 | 25 | |
Kifunensine inhibits mannosidase I, leading to the accumulation of high-mannose glycans. This accumulation can inhibit DPM2 activity by disrupting the normal processing and maturation of glycoproteins, a process that DPM2 is directly involved in through its function in the glycosylation pathway. | ||||||
Brefeldin A | 20350-15-6 | sc-200861C sc-200861 sc-200861A sc-200861B | 1 mg 5 mg 25 mg 100 mg | $30.00 $52.00 $122.00 $367.00 | 25 | |
Brefeldin A disrupts the Golgi apparatus structure and function, which is essential for glycoprotein processing and transport. As DPM2 is involved in the synthesis of dolichol-linked oligosaccharides in the ER-Golgi network, disruption caused by Brefeldin A can lead to functional inhibition of DPM2 by impairing the environment necessary for its activity. | ||||||
N-Butyldeoxynojirimycin·HCl | 210110-90-0 | sc-201398 sc-201398A sc-201398B | 5 mg 25 mg 50 mg | $148.00 $492.00 $928.00 | 4 | |
N-butyldeoxynojirimycin inhibits glucosidase I and II, which are critical for proper protein folding and glycan processing. Inhibition of these enzymes indirectly inhibits DPM2 by disrupting the glycosylation process that is essential for DPM2's role in the formation of glycoproteins. | ||||||
Celgosivir | 121104-96-9 | sc-488385 sc-488385A sc-488385B | 5 mg 25 mg 100 mg | $525.00 $902.00 $2700.00 | ||
Celgosivir is a prodrug of castanospermine and an inhibitor of alpha-glucosidases I and II. As with castanospermine, it can indirectly inhibit DPM2 by blocking the enzymes crucial for the first steps of glycoprotein glycosylation, a process in which DPM2 is involved. | ||||||